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抑制剂/激活剂

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凋亡与自噬

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ABT-737

ABT-737是一种BH3模拟抑制剂，作用于Bcl-xL，Bcl-2和Bcl-w，无细胞试验中EC50分别为78.7 nM，30.3 nM和197.8 nM；但对Mcl-1， Bcl-B及Bfl-1没有抑制作用。ABT-737可诱导线粒体通路的凋亡和线粒体自噬。Phase 2。

货号：
TK0164
规格：

5mg

10mg
价格：
￥0.00

产品参数

CAS No.	852808-04-9
生物活性	ABT-737, a BH3 mimetic, is a potent Bcl-2, Bcl-xL and Bcl-w inhibitor with EC50s of 30.3 nM, 78.7 nM, and 197.8 nM, respectively. ABT-737 induces the disruption of the BCL-2/BAX complex and BAK-dependent but BIM-independent activation of the intrinsic apoptotic pathway. ABT-737 induces autophagy and has the potential for acute myeloid leukemia (AML) research.
分子式	C42H45ClN6O5S2
分子量	813.43
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20℃ 3 years
溶解性数据	DMSO : 66.67 mg/mL (81.96 mM; ultrasonic and warming and heat to 60°C)
体内研究	ABT-737 (20, 30 mg/kg/day; i.p.; for 21 days) suppresses the leukemia burden by 48% and 53% at the 20 and 30 mg/kg dose levels, respectively, in four- to six-week-old CB.17 Scid mice with human leukemia KG-1 cells. ABT-737 significantly extends survival of mice in this aggressive leukemia model.
体外研究	ABT-737 binds BCL-2, BCL-XL, and BCL-W with high affinity (Ki<1 nM) but binds weakly (Ki>460 nM) to other antiapoptotic BCL-2 family members, including MCL-1 and BFL-1. ABT-737 binds the BH3-binding groove of BCL-XL and BCL-2. ABT-737 (100 nM; 1-72 hours) induces apoptosis and synergizes with chemotherapy in HL-60 cells. ABT-737 (5, 7.5, 10 μM; 72 hours) causes approximately 80% HCT116 cell death. The BAX knockout variant is completely resistant to ABT-737. ABT-737 has no effect on cell cycle distribution. ABT-737 disrupts BCL-2/BAX heterodimerization and induces BAX conformational change in HL-60 leukemic cells. ABT-737 induces a BAX/BAK-dependent impairment of maximal O2 consumption rate in sensitive cells. Stable BCL-2 overexpression in MCF10A cells induces an ABT-737-sensitive primed for death state. ABT-737 induces dose-dependent impairment of maximal O2 consumption rate in B-cell lymphoma cells.
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纯度及产品资料	98%

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